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Ten things you should know about protein kinases: IUPHAR Review 14
Doriano Fabbro1, Sandra W Cowan-Jacob2, Henrik Moebitz2
1PIQUR Therapeutics, Basel, Switzerland.
Abstract:
Many human malignancies are associated with aberrant regulation of protein or lipid kinases due to mutations, chromosomal rearrangements and/or gene amplification. Protein and lipid kinases represent an important target class for treating human disorders. This review focus on 'the 10 things you should know about protein kinases and their inhibitors', including a short introduction on the history of protein kinases and their inhibitors and ending with a perspective on kinase drug discovery. Although the '10 things' have been, to a certain extent, chosen arbitrarily, they cover in a comprehensive way the past and present efforts in kinase drug discovery and summarize the status quo of the current kinase inhibitors as well as knowledge about kinase structure and binding modes. Besides describing the potentials of protein kinase inhibitors as drugs, this review also focus on their limitations, particularly on how to circumvent emerging resistance against kinase inhibitors in oncological indications.
Insights
Protein kinases are crucial in cancer, making them key drug targets. This review covers protein kinase inhibitors, their history, current status, and strategies to overcome resistance in cancer treatment.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Aberrant regulation of protein and lipid kinases is implicated in numerous human cancers.
- Protein and lipid kinases are vital therapeutic targets for various human disorders.
- Kinase dysregulation arises from mutations, chromosomal rearrangements, and gene amplification.
Purpose of the Study:
- To provide a comprehensive overview of protein kinases and their inhibitors.
- To cover the history, current state, and future perspectives of kinase drug discovery.
- To discuss the potential and limitations of protein kinase inhibitors in oncological indications.
Main Methods:
- Literature review focusing on protein kinase inhibitors.
- Analysis of historical developments and current advancements in kinase drug discovery.
- Examination of kinase structure, binding modes, and resistance mechanisms.
Main Results:
- Protein kinases are central to many human malignancies.
- Kinase inhibitors show significant therapeutic potential but face limitations.
- Emerging resistance to kinase inhibitors is a critical challenge in oncology.
Conclusions:
- Protein kinase inhibitors represent a significant advancement in cancer therapy.
- Understanding kinase structure and function is key to drug development.
- Strategies to overcome resistance are essential for sustained efficacy of kinase inhibitors.
